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Page 1
Discovery of Ecopladib, an indole inhibitor of cytosolic phospholipase A2alpha.
Lee KL, Foley MA, Chen L, Behnke ML, Lovering FE, Kirincich SJ, Wang W, Shim J, Tam S, Shen MW, Khor S, Xu X, Goodwin DG, Ramarao MK, Nickerson-Nutter C, Donahue F, Ku MS, Clark JD, McKew JC. Lee KL, et al. Among authors: xu x. J Med Chem. 2007 Mar 22;50(6):1380-400. doi: 10.1021/jm061131z. Epub 2007 Feb 17. J Med Chem. 2007. PMID: 17305324
Benzenesulfonamide indole inhibitors of cytosolic phospholipase A2alpha: optimization of in vitro potency and rat pharmacokinetics for oral efficacy.
Lee KL, Behnke ML, Foley MA, Chen L, Wang W, Vargas R, Nunez J, Tam S, Mollova N, Xu X, Shen MW, Ramarao MK, Goodwin DG, Nickerson-Nutter CL, Abraham WM, Williams C, Clark JD, McKew JC. Lee KL, et al. Among authors: xu x. Bioorg Med Chem. 2008 Feb 1;16(3):1345-58. doi: 10.1016/j.bmc.2007.10.060. Epub 2007 Oct 22. Bioorg Med Chem. 2008. PMID: 17998165
Indole cytosolic phospholipase A2 alpha inhibitors: discovery and in vitro and in vivo characterization of 4-{3-[5-chloro-2-(2-{[(3,4-dichlorobenzyl)sulfonyl]amino}ethyl)-1-(diphenylmethyl)-1H-indol-3-yl]propyl}benzoic acid, efipladib.
McKew JC, Lee KL, Shen MW, Thakker P, Foley MA, Behnke ML, Hu B, Sum FW, Tam S, Hu Y, Chen L, Kirincich SJ, Michalak R, Thomason J, Ipek M, Wu K, Wooder L, Ramarao MK, Murphy EA, Goodwin DG, Albert L, Xu X, Donahue F, Ku MS, Keith J, Nickerson-Nutter CL, Abraham WM, Williams C, Hegen M, Clark JD. McKew JC, et al. Among authors: xu x. J Med Chem. 2008 Jun 26;51(12):3388-413. doi: 10.1021/jm701467e. Epub 2008 May 23. J Med Chem. 2008. PMID: 18498150
Piperazine sulfonamides as potent, selective, and orally available 11beta-hydroxysteroid dehydrogenase type 1 inhibitors with efficacy in the rat cortisone-induced hyperinsulinemia model.
Xiang J, Wan ZK, Li HQ, Ipek M, Binnun E, Nunez J, Chen L, McKew JC, Mansour TS, Xu X, Suri V, Tam M, Xing Y, Li X, Hahm S, Tobin J, Saiah E. Xiang J, et al. Among authors: xu x. J Med Chem. 2008 Jul 24;51(14):4068-71. doi: 10.1021/jm8004948. Epub 2008 Jun 26. J Med Chem. 2008. PMID: 18578516
Discovery of potent and selective matrix metalloprotease 12 inhibitors for the potential treatment of chronic obstructive pulmonary disease (COPD).
Wu Y, Li J, Wu J, Morgan P, Xu X, Rancati F, Vallese S, Raveglia L, Hotchandani R, Fuller N, Bard J, Cunningham K, Fish S, Krykbaev R, Tam S, Goldman SJ, Williams C, Mansour TS, Saiah E, Sypek J, Li W. Wu Y, et al. Among authors: xu x. Bioorg Med Chem Lett. 2012 Jan 1;22(1):138-43. doi: 10.1016/j.bmcl.2011.11.046. Epub 2011 Nov 20. Bioorg Med Chem Lett. 2012. PMID: 22153340
Diazine indole acetic acids as potent, selective, and orally bioavailable antagonists of chemoattractant receptor homologous molecule expressed on Th2 cells (CRTH2) for the treatment of allergic inflammatory diseases.
Kaila N, Huang A, Moretto A, Follows B, Janz K, Lowe M, Thomason J, Mansour TS, Hubeau C, Page K, Morgan P, Fish S, Xu X, Williams C, Saiah E. Kaila N, et al. Among authors: xu x. J Med Chem. 2012 Jun 14;55(11):5088-109. doi: 10.1021/jm300007n. Epub 2012 May 31. J Med Chem. 2012. PMID: 22651823
Discovery of HSD-621 as a Potential Agent for the Treatment of Type 2 Diabetes.
Wan ZK, Chenail E, Li HQ, Ipek M, Xiang J, Suri V, Hahm S, Bard J, Svenson K, Xu X, Tian X, Wang M, Li X, Johnson CE, Qadri A, Panza D, Perreault M, Mansour TS, Tobin JF, Saiah E. Wan ZK, et al. Among authors: xu x. ACS Med Chem Lett. 2012 Nov 23;4(1):118-23. doi: 10.1021/ml300352x. eCollection 2013 Jan 10. ACS Med Chem Lett. 2012. PMID: 24900572 Free PMC article.
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